AZD 2858
Tocris Bioscience, part of Bio-Techne | Catalog # 7650
Highly potent GSK-3 inhibitor; inhibits tau phosphorylation
Key Product Details
Description
Highly potent GSK-3 inhibitor; inhibits tau phosphorylation
Product Description
AZD 2858 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 values are 0.9 and 5 nM for GSK-3α and GSK-3β, respectively). AZD 2858 inhibits tau phosphorylation in vitro (IC50 = 76 nM), improves fracture healing and increases bone mass in rodent models of bone fracture. Also activates Wnt signaling in vitro and in vivo. Brain permeable and orally bioavailable.Product Specifications
Molecular Weight
453.52
Formula
C21H23N7O3S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide
CAS Number
486424-20-8
PubChem ID
10138980
InChI Key
FHCSBLWRGCOVPT-UHFFFAOYSA-N
SMILES
O=C(NC=1C=NC=CC1)C=2N=C(C=NC2N)C3=CC=C(C=C3)S(=O)(=O)N4CCN(C)CC4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.54 | 10 |
Preparing Stock Solutions
for AZD 2858
The following data is based on the product molecular weight 453.52
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 22.05 mL | 110.25 mL | 220.50 mL |
| 0.5 mM | 4.41 mL | 22.05 mL | 44.10 mL |
| 1 mM | 2.20 mL | 11.02 mL | 22.05 mL |
| 5 mM | 0.44 mL | 2.20 mL | 4.41 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Berg Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines. J.Med.Chem. 2012 PMID: 22489897
- Cook Wnt-dependent osteogenic commitment of bone marrow stromal cells using a novel GSK3β inhibitor. Stem Cell Res. 2014 PMID: 24382458
- Sisask Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone 2013 PMID: 23337038
Product Specific Notices for AZD 2858
For research use only
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